An overview of molecular hybrids in drug discovery

ABSTRACT

Introduction: The hybridization of biologically active molecules is a powerful tool for drug discovery used to target a variety of diseases. It offers the prospect of better drugs for the treatment of a number of illnesses including cancer, malaria, tuberculosis and AIDS. Hybrid drugs can provide combination therapies in a single multi-functional agent and, by doing so, be more specific and powerful than conventional classic treatments. This research field is in great expansion and attracts many researchers worldwide.

Area covered: This review covers the main research published between early 2013 to mid-2015 and takes into account several previous reviews on the subject. Its intention is to showcase the most recent advances reported towards the development of molecular hybrids in drug discovery. Particular attention is given to anticancer hybrids throughout the review.

Expert opinion: Current advances show that molecular hybrids of biologically active molecules can lead to powerful therapeutics. Natural products play a key role in this field. It is also believed that toxin hybrids present a great opportunity for future progress and should be further explored. Furthermore, the synthesis of hybrid organometallics should be systematically studied as it can lead to potent drugs. The crucial requirement for growth still remains the efficacy of synthesis. Hence, the development of efficient synthetic methods allowing rapid access to diverse series of hybrids must be further investigated by researchers.

KEYWORDS:

• Drug design
• drug-targeting
• molecular hybrids
• anticancer agents

Article highlights

• Research on molecular hybrids is gaining momentum worldwide showing their promise in drug discovery.

• Natural products play a key role for the design of molecular hybrids.

• Multicomponent reactions and/or click chemistry are important synthetic tools to synthesize hybrids.

• Hybrids comprising an organometallic component are likely to exhibit significant biological properties.

• Toxins can be lethal but display great potential to access potent anticancer hybrids.

This box summarizes key points contained in the article.

Financial & Competing Interests Disclosure

G Berube thanks the Université du Québec à Trois-Rivières for financial support. He has no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.